EFFECT OF PAZUFLOXACIN MESILATE, A NEW QUINOLONE ANTIBACTERIAL AGENT FOR INTRAVENOUS USE, ON QT INTERVAL

• Published in: Japanese journal of antibiotics 2004/08/25, Vol.57(4), pp.404-412
• Main Authors: FUKUDA, HITOSHI, MORITA, YUKIE, SHIOTANI, NORIO, MIZUO, MIDORI, KOMAE, NORIHISA
• Format: Article
• Language: Japanese
• Subjects: Animals; Anti-Bacterial Agents - administration & dosage; Anti-Bacterial Agents - adverse effects; Dogs; Electrocardiography - drug effects; Female; Fluoroquinolones - administration & dosage; Fluoroquinolones - adverse effects; Guinea Pigs; In Vitro Techniques; Injections, Intravenous; Long QT Syndrome; Male; Membrane Potentials - drug effects; Oxazines - administration & dosage; Oxazines - adverse effects; Papillary Muscles - drug effects; Quinolones - administration & dosage; Quinolones - adverse effects
• ISSN: 0368-2781; 2186-5477
• DOI: 10.11553/antibiotics1968b.57.404

The potential for QT interval prolongation of pazufloxacin mesilate (PZFX mesilate), a new quinolone antibacterial agent for intravenous use, was investigated by in vitro and in vivo electrophysiology studies. Following results were obtained. In vitro electrophysiology study using guinea pig papillary muscles: PZFX mesilate (30-300μm) had no effects on resting membrane potential (RMP), action potential amplitude (APA) and action potential duration (APD). Reference quinolones, sparfloxacin (3-30μM) and moxifloxacin (10-100μm), had no effects on RMP and APA, but significantly prolonged APD at more than 3 and 10 μM, respectively, while ciprofloxacin 10-100μm) had no effect on each parameter. In vivo electrophysiology study using anesthetized dogs: PZFX mesilate had no effects on electrocardiograph parameter (PR interval, QRS interval, QT interval and QTc) after intravenous administration of 3-30 mg/kg. These results suggest that PZFX mesilate has low potential for QT interval prolongation.